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Dr. Ignacio Delso Dr. Jessika Valero‐Gonzalez Dr. Fernando Gomollón‐Bel Jorge Castro‐López Dr. Wenxia Fang Dr. Iva Navratilova Prof. Daan M. F. van Aalten Prof. Tomás Tejero Prof. Pedro Merino Dr. Ramon Hurtado‐Guerrero 《ChemMedChem》2018,13(2):128-132
Fungal β‐1,3‐glucan glucanosyltransferases are glucan‐remodeling enzymes that play important roles in cell wall integrity, and are essential for the viability of pathogenic fungi and yeasts. As such, they are considered possible drug targets, although inhibitors of this class of enzymes have not yet been reported. Herein we report a multidisciplinary approach based on a structure‐guided design using a highly conserved transglycosylase from Sacharomyces cerevisiae, that leads to carbohydrate derivatives with high affinity for Aspergillus fumigatus Gel4. We demonstrate by X‐ray crystallography that the compounds bind in the active site of Gas2/Gel4 and interact with the catalytic machinery. The topological analysis of noncovalent interactions demonstrates that the combination of a triazole with positively charged aromatic moieties are important for optimal interactions with Gas2/Gel4 through unusual pyridinium cation–π and face‐to‐face π–π interactions. The lead compound is capable of inhibiting AfGel4 with an IC50 value of 42 μm . 相似文献
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Microbial Fuel Cell Application for Azoic Dye Decolorization with Simultaneous Bioenergy Production Using Stenotrophomonas sp. 下载免费PDF全文
Said Galai Antonia Pérez de los Ríos Francisco José Hernández‐Fernández Sihem Haj Kacem Francisco Mateo Ramírez Joaquín Quesada‐Medina 《化学工程与技术》2015,38(9):1511-1518
A single‐chamber air‐cathode microbial fuel cell (MFC) was successfully applied for decolorization of the diazoic dye Reactive Black 5 (RB5) with simultaneous production of electricity. An innovative low‐cost medium, the marine water‐glucose‐yeast extract medium (MWGY), was developed which appears as a textile marine effluent in terms of salinity. The anode compartment containing a single bacterial strain of Stenotrophomonas sp. showed almost complete dye decolorization with different RB5 concentrations after seven days of treatment. For the four dye concentrations used, a correlation between dye removal and production of electrical energy was found. The comparison of the decolorization process in the MFC with that in a batch reactor as control experiment highlights the efficiency of the single‐chamber air‐cathode MFC technology which improved the dye removal by the same bacterial strain. 相似文献
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Cellular Antisense Activity of PNA–Oligo(bicycloguanidinium) Conjugates Forming Self‐Assembled Nanoaggregates 下载免费PDF全文
Dr. Julián Valero Dr. Takehiko Shiraishi Prof. Javier de Mendoza Prof. Peter E. Nielsen 《Chembiochem : a European journal of chemical biology》2015,16(11):1593-1600
A series of peptide nucleic acid–oligo(bicycloguanidinium) (PNA–BGn) conjugates were synthesized and characterized in terms of cellular antisense activity by using the pLuc750HeLa cell splice correction assay. PNA–BG4 conjugates exhibited low micromolar antisense activity, and their cellular activity required the presence of a hydrophobic silyl terminal protecting group on the oligo(BG) ligand and a minimum of four guanidinium units. Surprisingly, a nonlinear dose–response with an activity threshold around 3–4 μM , indicative of large cooperativity, was observed. Supported by light scattering and electron microscopy analyses, we propose that the activity, and thus cellular delivery, of these lipo‐PNA–BG4 conjugates is dependent on self‐assembled nanoaggregates. Finally, cellular activity was enhanced by the presence of serum. Therefore we conclude that the lipo‐BG‐PNA conjugates exhibit an unexpected mechanism for cell delivery and are of interest for further in vivo studies. 相似文献
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Carolina Blanco Raúl Bodas Sonia Andrés Jose María Rodríguez-Calleja Javier Mateo Fernando Rozada F. Javier Giráldez 《International Journal of Food Science & Technology》2020,55(3):1119-1125
Thirty-two lambs were finished on a total mixed ration (TMR) pelleted alone (00SS) or including sunflower soap stock (SS): 15SS (15 g SS per kg TMR), 30SS (30 g SS per kg TMR) and 60SS (60 g SS per kg TMR). Lambs (8 per group) were slaughtered at 27 kg live weight. Colour evolution, lipid oxidation, microbial growth and detection of diarrhoeagenic Escherichia coli were studied in meat samples. SS in the diet reduced meat lipid oxidation (P < 0.05), but had no significant effect (P > 0.05) on the cholesterol oxidation products. Meat from 60SS and control animals (00SS) revealed greater discoloration (P < 0.05) than 15SS. SS supplementation did not affect the microbiological populations, whereas high doses of SS seemed to increase the proliferation of diarrhoeagenic E. coli on day 14 (P < 0.10). These results suggest that the rate of SS inclusion in the diet of fattening lambs should not be above 15 g SS per kg TMR. 相似文献
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